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积雪草酸衍生物的合成与表征及体外抗癌活性的研究
引用本文:赵龙铉,田明珠,金礼吉,贺兴隆,沈平,张晓翠,杨君微.积雪草酸衍生物的合成与表征及体外抗癌活性的研究[J].有机化学,2011,31(5).
作者姓名:赵龙铉  田明珠  金礼吉  贺兴隆  沈平  张晓翠  杨君微
作者单位:1. 辽宁师范大学化学化工学院,大连,116029;辽宁师范大学生物技术与分子药物研发辽宁省重点实验室,大连,116029
2. 辽宁师范大学化学化工学院,大连,116029
3. 大连理工大学环境与生命学院,大连,116029
摘    要:为了寻找新型高效、低毒、生物活性良好的积雪草酸衍生物,以具有一定生物活性的积雪草酸为先导化合物,通过对其C-2,C-3,C-11,C-23和C-28位进行结构修饰,设计合成了9种未见文献报道的积雪草酸衍生物.目标化合物的结构经1H NMR,13C NMR,IR和HRMS表征确证.采用MTT法观察其对人宫颈癌细胞(Hela)、人乳腺癌细胞(MCF-7)的抑制作用.结果表明,经修饰的积雪草酸衍生物的抗癌活性较母体化合物有不同程度的增强.

关 键 词:积雪草酸  衍生物  合成  表征  抗癌

Synthesis and Characterization of Derivatives of Asiatic Acid and Primary Study on Anti-cancer Activity
Zhao Longxuan,Tian Mingzhu,Jin Liji,He Xinglong,Shen Ping,Zhang Xiaocui,Yang Junwei.Synthesis and Characterization of Derivatives of Asiatic Acid and Primary Study on Anti-cancer Activity[J].Chinese Journal of Organic Chemistry,2011,31(5).
Authors:Zhao Longxuan  Tian Mingzhu  Jin Liji  He Xinglong  Shen Ping  Zhang Xiaocui  Yang Junwei
Institution:Zhao,Longxuan*,a,b Tian,Mingzhua Jin,Lijic He,Xinglonga Shen,Pinga Zhang,Xiaocuia Yang,Junweia(a School of Chemistry and Chemical Engineering,Liaoning Normal University,Dalian 116029)(b Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery,Dalian 116029)(c School of Environmental & Biological Science & Technology,Dalian University of Technology,Dalian 116029)
Abstract:In order to develop novel asiatic acid derivatives with high efficiency,low toxicity and good biological activity,we used natural product asiatic acid as the lead compound,which exhibits anti-cancer ac-tivity.Nine novel asiatic acid derivatives were designed and synthesized through modification of asiatic acid at C-2,C-3,C-11,C-23 and C-28.Structures of all target compounds were confirmed by 1H NMR,13C NMR,IR and HRMS techniques.Their in vitro anti-cancer activities towards Hela cell and MCF-7 cell lines we...
Keywords:asiatic acid  derivative  synthesis  characterization  anti-cancer  
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